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Literature summary for 5.6.2.2 extracted from
- Decreased nucleotide excision repair activity and alterations of topoisomerase IIalpha are associated with the in vivo resistance of a P388 leukemia subline to F11782, a novel catalytic inhibitor of topoisomerases I and II (2004), Clin. Cancer Res., 10, 3156-3168.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| DNA sequence determination and analysis of the P388/F11782 cell and the P338 cell enzymes | Mus musculus |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 1,3-bis(2-chloroethyl)-1-nitroso-urea | P388/F11782 cell enzyme, high inhibition | Mus musculus |  |
| 5-fluorouracil | P388/F11782 cell enzyme, high inhibition | Mus musculus | |
| camptothecin | P388/F11782 cell enzyme, high inhibition | Mus musculus | |
| cisplatin | P388/F11782 cell enzyme, high inhibition | Mus musculus | |
| Colchicine | P388/F11782 cell enzyme, high inhibition | Mus musculus | |
| cyclophosphamide | P388/F11782 cell enzyme, high inhibition | Mus musculus | |
| etopophos | P388/F11782 cell enzyme, high inhibition | Mus musculus | |
| etoposide | P388/F11782 cell enzyme, low inhibition | Mus musculus | |
| F11782 | inhibition of the P388 cell enzyme, mechanism, in vitro resistance of the P388/F11782 cell enzyme to the inhibitor is not associated with a classic multidrug resistance profile, resistant cells show cross-resistance to merbarone and doxorubicin, resistance mechanism | Mus musculus | |
| irinotecan | P388/F11782 cell enzyme, high inhibition | Mus musculus | |
| methotrexate | P388/F11782 cell enzyme, low inhibition | Mus musculus | |
| mitoxanthrone | P388/F11782 cell enzyme, high inhibition | Mus musculus | |
| additional information | P388/F11782 cells, resistant to F11782, show cross-resistance to merbarone and doxorubicin | Mus musculus | |
| TAS-103 | P388/F11782 cell enzyme, low inhibition | Mus musculus | |
| Teniposide | P388/F11782 cell enzyme, high inhibition | Mus musculus | |
| topotecan | P388/F11782 cell enzyme, high inhibition | Mus musculus | |
| vinblastine | P388/F11782 cell enzyme, high inhibition | Mus musculus | |
| vinflunine | P388/F11782 cell enzyme, high inhibition | Mus musculus | |
| vinorelbine | P388/F11782 cell enzyme, high inhibition | Mus musculus | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | - |
Mus musculus | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Mus musculus | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| P-388 cell | F11782-resistant P388 leukemia subline P388/F11782, development of the F11782-resistant subclone of P338 leukemia cell line, the cells show reduced enzyme amount and activity | Mus musculus | - |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| additional information | - |
F11782-resistant cells show reduced enzyme amount and activity | Mus musculus |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| kinetoplast DNA + ATP + H2O | decatenation of kinetoplast DNA | Mus musculus | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| topoisomerase IIalpha | - |
Mus musculus |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Mus musculus |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 8 | - |
assay at | Mus musculus |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Mus musculus | |
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